The Chalcogen Is Bonded Directly To A Ring Carbon Of The Five-membered Hetero Ring Which Is Adjacent To The Ring Nitrogen (e.g., 2-indolinones, Etc.) Patents (Class 548/486)
  • Patent number: 10065926
    Abstract: The invention relates to the use of substituted dihydrooxindolylsulfonamides or salts thereof of the formula (I) where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, and/or for increasing plant yield.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: September 4, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Jens Frackenpohl, Guido Bojack, Hendrik Helmke, Stefan Lehr, Thomas Mueller, Lothar Willms, Jan Dittgen, Dirk Schmutzler, Udo Bickers, Harry Strek, Rachel Baltz
  • Patent number: 9017922
    Abstract: A chemically amplified resist composition comprising a base polymer and an amine quencher in the form of a ?-alanine, ?-aminobutyric acid, 5-aminovaleric acid, 6-aminocaproic acid, 7-aminoheptanoic acid. 8-aminooctanoic acid or 9-aminononanoic acid derivative having an unsubstituted carboxyl group has a high contrast of alkaline dissolution in rate before and after exposure and forms a pattern of good profile at a high resolution, minimal roughness and wide DOF.
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: April 28, 2015
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Jun Hatakeyama, Masayoshi Sagehashi
  • Publication number: 20150051260
    Abstract: Compounds, compositions and methods relating to EWS-FLI1 protein inhibitors are provided. The compounds have utility in the treatment of cancers including the Ewing's sarcoma family of tumors.
    Type: Application
    Filed: April 11, 2013
    Publication date: February 19, 2015
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Jeffrey A. Toretsky, Milton Lang Brown, Perrer N. Tosso, Aykut Uren, Yali Kong
  • Publication number: 20150045395
    Abstract: This invention relates to methods of reversing and inhibiting liver fibrosis and hepatitis using a small indolinone molecule Hesperadin and related compounds. Methods of identifying such agents and using them to inhibit the expression of collagens and ECM proteins including MMPs and TIMPs in purified hepatic stellate cells are provided. In vivo data of Hesperadin in inhibiting induced collagen production are presented. This method of specifically targeting drugs to hepatic stellate cells in vivo, provides a novel therapy for liver diseases.
    Type: Application
    Filed: August 9, 2013
    Publication date: February 12, 2015
    Applicant: Acclaim BioMed USA LLC
    Inventors: Kenneth Ka-Ho Lee, Stanton Hon-Lung Kok, Tsz-Wai Kok, Sing-Wan Wong, John Yeuk-Hon Chan
  • Patent number: 8937095
    Abstract: The invention describes dual Aurora kinase/MEK inhibitors and their use in therapy.
    Type: Grant
    Filed: July 9, 2013
    Date of Patent: January 20, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephan Karl Zahn, Patrizia Sini, Bojan Bister
  • Publication number: 20140371446
    Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) methods of using such phosphacycle ligands in bond forming reactions; and (c) methods of preparing phosphacycle ligands.
    Type: Application
    Filed: August 25, 2014
    Publication date: December 18, 2014
    Applicant: AbbVie Inc.
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Patent number: 8877946
    Abstract: Compounds of general formula I: wherein R1a, R1b, R2, R3a, R3b and X are as defined herein are tyrosine kinase inhibitors and are useful for the treatment of various diseases and conditions, for example cancer.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: November 4, 2014
    Assignee: National University of Singapore
    Inventors: Mei Lin Go, Han Kiat Ho, Xiao Chen
  • Patent number: 8853420
    Abstract: The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: July 28, 2009
    Date of Patent: October 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Treu, Thomas Karner, Ulrich Reiser
  • Publication number: 20140296292
    Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 2, 2014
    Inventors: Lin Zhi, Keith Marschke, Virginia H. Grant, Steven L. Roach, Yixing Shen, Jason C. Pickens, Bijan Pedram, C. Arjan van Oeveren, Lino J. Valdez, Andrew R. Hudson
  • Publication number: 20140275075
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 18, 2014
    Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
  • Publication number: 20140249199
    Abstract: The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula (I), pharmaceutical compositions having a compound of formula (I), and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula (I) to a subject in need thereof.
    Type: Application
    Filed: July 19, 2012
    Publication date: September 4, 2014
    Applicants: HEALTH RESEARCH, INC., EMORY UNIVERSITY
    Inventors: Huw M. L. Davies, Spandan Chennamadhavuni, Andrei Bakin
  • Publication number: 20140249148
    Abstract: Provided herein are inhibitors of HDAC3, as well as methods of treatment comprising administering those compounds to a subject in need thereof.
    Type: Application
    Filed: January 31, 2014
    Publication date: September 4, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20140221450
    Abstract: The present invention relates to a composition comprising a maxi-K potassium channel opener the use in the treatment of fragile X syndrome. More specifically the present invention relates to a composition comprising a fluoro-oxindole or a chloro-oxindole for use in the treatment of fragile X syndrome.
    Type: Application
    Filed: June 19, 2012
    Publication date: August 7, 2014
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE D'ORLEANS, CENTRE HOSPITALIER REGIONAL D'ORLEANS
    Inventors: Sylvain Briault, Olivier Perche
  • Patent number: 8772288
    Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: July 8, 2014
    Assignee: Almirall, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
  • Patent number: 8758880
    Abstract: Monomeric or polymeric compounds comprising at least one moiety of the formula (Ia) wherein X is CR, where R is H or a substituent as defined in claim 1, or is another ketopyrrole moiety e.g. of the formula (Ib) or (Ic) with this moiety and all other symbols are as defined in claim 1, show good solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers according to the invention are used in semiconductor devices or organic photovoltaic (PV) devices (solar cells).
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: June 24, 2014
    Assignee: BASF SE
    Inventors: Jean-Charles Flores, Ulrich Berens, Frank Bienewald, Hans Jürg Kirner, Mathieu G. R. Turbiez
  • Patent number: 8722723
    Abstract: A compound represented by the following general formula (I) (R1 and R2 represent hydrogen atom, an alkyl group, a halogen atom, etc.; R3 and R4 represent hydrogen atom, an alkyl group, an alkoxy group, or an alkenyl group; R5 represents hydrogen atom, an alkyl group, or nitro group, and R6 represents hydrogen atom or an alkyl group), which acts on the transcription process of genes.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: May 13, 2014
    Assignee: Research Foundation Itsuu Laboratory
    Inventors: Nobuko Fujimaki, Madoka Nakagomi, Koichi Shudo
  • Patent number: 8680135
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: March 25, 2014
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
  • Publication number: 20140024678
    Abstract: The subject invention provides a pharmaceutical composition comprising N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5- chloro-1-methyl-2-oxoquinoline-3-carboxamide or the salt thereof; a pharmaceutically acceptable carrier; and not more than 0.5% w/w relative to N-ethyl-N-phenyl-1,2,-dihydro-4 -hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide of 2-Chloro-6-(1-ethyl-N-methyl-2-oxoindoline-3-carboxamido) benzoic acid, 1H,3H-spiro[5-chloro-1-methylquinoline-2,4 -dione-3,3?-[1]ethylindolin-[2]-one], or 5-Chloro-N-ethyl-3-hydroxy-1-methyl-2,4-dioxo-N-phenyl-1,2,3,4 -tetrahydro-quinoline-3-carboxamide.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Muhammad Safadi, Daniella Licht, Ioana Lovinger, Aharon M. Eyal, Tomas Fristedt, Karl Jansson
  • Publication number: 20140018405
    Abstract: The invention describes dual Aurora kinase/MEK inhibitors and their use in therapy.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 16, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan Karl ZAHN, Patrizia SINI, Bojan BISTER
  • Publication number: 20140018372
    Abstract: A crystalline form of 3-{3-[1-(4-Dimethylaminomethyl-phenylamino)-1-phenyl-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indol-6-yl}-propynoic acid ethylamide.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 16, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerd-Michael MAIER, Anke BAUM, Bodo BETZEMEIER, Manuel HENRY, Rolf HERTER, Ulrich REISER, Patrizia SINI, Dirk WEBER, Ulrike WERTHMANN, Stephan Karl ZAHN
  • Patent number: 8629141
    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: January 14, 2014
    Assignees: The Regents of the University of Michigan, Sanofi
    Inventors: Shaomeng Wang, Wei Sun, Angelo Aguilar, Carlos Garcia-Echeverria
  • Publication number: 20130344165
    Abstract: This disclosure relates to compounds and compositions for forming bone and methods related thereto. In certain embodiments, the disclosure relates to methods of forming bone comprising implanting a bone graft composition comprising a growth factor such as BMP in a subject at a site of desired bone growth or enhancement in combination with a JAB1 blocker.
    Type: Application
    Filed: February 23, 2012
    Publication date: December 26, 2013
    Applicant: EMORY UNIVERSITY
    Inventors: Scott D. Boden, Sreedhara Sangadala
  • Publication number: 20130281451
    Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.
    Type: Application
    Filed: April 3, 2013
    Publication date: October 24, 2013
    Applicant: ANNJI PHARMACEUTICAL CO., LTD.
    Inventors: Ji-Wang Chern, Ajit Dhananjay Jagtap, Hsiao-Chun Wang, Grace Shiahuy Chen
  • Patent number: 8563749
    Abstract: Process for preparing 1,3-dihydro-2H-indol-2-ones, starting from thioalkyl-, or thiocycloalkyl-substituted indol-2-one compounds, involving a) dissolving or suspending the thioalkyl-, or thiocycloalkyl-substituted indol-2-one compounds in a polar solvent, b) adding a sulfur-containing salt to the solution or suspension, and c) heating the reaction mixture under reflux at a temperature which corresponds at most to the boiling temperature of the solvent. Use of the inventively prepared 1,3-dihydro-2H-indol-2-one as intermediates for the synthesis of fine chemicals and active ingredients from pharmacy and/or agriculture.
    Type: Grant
    Filed: May 9, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Konrad Siegel, Gunter Karig
  • Publication number: 20130274483
    Abstract: This invention is directed to asymmetric syntheses of certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: March 11, 2013
    Publication date: October 17, 2013
    Inventors: Shaoyi Sun, Jianmin Fu, Sultan Chowdhury, Ivan William Hemeon, Michael Edward Grimwood, Tarek Suhayl Mansour
  • Patent number: 8546443
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R5 to R10, A, L1, B, m and p are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: October 1, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Treu, Stephan Karl Zahn, Patricia Amouzegh, Cristina Lecci, Heather Tye
  • Patent number: 8545885
    Abstract: The subject invention provides a pharmaceutical composition comprising N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide or the salt thereof; a pharmaceutically acceptable carrier; and not more than 0.5% w/w relative to N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide of 2-Chloro-6-(1-ethyl-N-methyl-2-oxoindoline-3-carboxamido)benzoic acid, 1H,3H-spiro[5-chloro-1-methylquinoline-2,4-dione-3,3?-[1]ethylindolin-[2]-one], or 5-Chloro-N-ethyl-3-hydroxy-1-methyl-2,4-dioxo-N-phenyl-1,2,3,4-tetrahydro-quinoline-3-carboxamide.
    Type: Grant
    Filed: May 14, 2012
    Date of Patent: October 1, 2013
    Assignees: Teva Pharmaceutical Industries, Ltd., Active Biotech, AB
    Inventors: Muhammad Safadi, Daniella Licht, Ioana Lovinger, Aharon M. Eyal, Tomas Fristedt, Karl Jansson
  • Publication number: 20130217876
    Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions.
    Type: Application
    Filed: August 21, 2012
    Publication date: August 22, 2013
    Applicant: ABBVIE INC.
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Publication number: 20130109672
    Abstract: Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2 (I).
    Type: Application
    Filed: April 26, 2011
    Publication date: May 2, 2013
    Applicant: The United States of America,as represented by the Secretary, Department of Health and Human Service
    Inventors: Matthew B. Boxer, Min Shen, Douglas S. Auld, Craig J. Thomas, Martin J. Walsh
  • Publication number: 20130102774
    Abstract: A process for transforming a group >C?O (I) in a compound into a group >C?S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2 C5H5N.
    Type: Application
    Filed: February 3, 2012
    Publication date: April 25, 2013
    Applicant: VIRONOVA AB
    Inventors: Birgitta Pettersson, Vedran Hasimbegovic, Per H Svensson, Jan Bergman
  • Publication number: 20130035364
    Abstract: Compounds of general formula I: wherein R1a, R1b, R2, R3a, R3b and X are as defined herein are tyrosine kinase inhibitors and are useful for the treatment of various diseases and conditions, for example cancer.
    Type: Application
    Filed: August 1, 2012
    Publication date: February 7, 2013
    Inventors: Mei Lin GO, Han Kiat HO, Xiao CHEN
  • Patent number: 8329686
    Abstract: Novel isatin analogues, including isatin analogues comprising Michael Acceptors (IMAs) are disclosed. Further disclosed are methods of synthesis of the isatin analogues, and uses of the analogues, including inhibition of caspase-3 and caspase-7, and in vivo imaging of apoptosis by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).
    Type: Grant
    Filed: August 29, 2007
    Date of Patent: December 11, 2012
    Assignee: Washington University
    Inventors: Robert H. Mach, Michael Welch, Wenhua Chu, Justin Rothfuss
  • Patent number: 8318793
    Abstract: The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: November 27, 2012
    Assignee: Abbott GmbH & Co. KG
    Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Wilfried Hornberger, Falko Ernst Wolter
  • Publication number: 20120253051
    Abstract: The present invention relates to an improved process for the preparation of Ropinirole and pharmaceutical acceptable salts or derivatives thereof, in particular to a process for large scale production of Ropinirole and salts thereof in high yield and high purity and pharmaceutical preparations containing said compounds.
    Type: Application
    Filed: December 16, 2009
    Publication date: October 4, 2012
    Applicant: PHARMATHEN S.A.
    Inventors: Theoharis V. Koftis, Ioanna Georgopoulou, Ravikant R. Soni, Panagiota Mandalou, Elli Alexandraki
  • Patent number: 8273749
    Abstract: A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Grant
    Filed: September 30, 2008
    Date of Patent: September 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Scott B. Hoyt, Clare London
  • Publication number: 20120225124
    Abstract: The subject invention provides a pharmaceutical composition comprising N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide or the salt thereof; a pharmaceutically acceptable carrier; and not more than 0.5% w/w relative to N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide of 2-Chloro-6-(1-ethyl-N-methyl-2-oxoindoline-3-carboxamido)benzoic acid, 1H,3H-spiro[5-chloro-1-methylquinoline-2,4-dione-3,3?-[1]ethylindolin-[2]-one], or 5-Chloro-N-ethyl-3-hydroxy-1-methyl-2,4-dioxo-N-phenyl-1,2,3,4-tetrahydro-quinoline-3-carboxamide.
    Type: Application
    Filed: May 14, 2012
    Publication date: September 6, 2012
    Inventors: Muhammad Safadi, Daniella Licht, Ioana Lovinger, Aharon M. Eyal, Tomas Fristedt, Karl Jansson
  • Patent number: 8211923
    Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: July 3, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Patent number: 8198313
    Abstract: This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: June 12, 2012
    Assignee: H. Lundbeck A/S
    Inventors: Michael Konkel, John M. Werzel, Jamie Talisman
  • Publication number: 20120142646
    Abstract: The present invention provides compounds of formula (I) wherein k, Ar, R2, R3, R4, R5, R4?, R5?, R6, R7, A, D, m and E are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 19, 2007
    Publication date: June 7, 2012
    Inventors: Lilian Alcaraz, Roger Victor Bonnert, Stephen Connolly, Anthony Ronald Cook, Adrian Fisher, Alexander Humphries, Piotr Raubo
  • Publication number: 20120141938
    Abstract: A chemically amplified resist composition comprising a base polymer, an acid generator, and an amine quencher in the form of a ?-alanine, ?-aminobutyric acid or 5-aminovaleric acid derivative having an acid labile group-substituted carboxyl group has a high contrast of alkaline dissolution rate before and after exposure and forms a pattern of good profile at a high resolution, minimal roughness and wide focus margin.
    Type: Application
    Filed: December 5, 2011
    Publication date: June 7, 2012
    Applicant: SHIN-ETSU CHEMICAL CO., LTD.
    Inventors: Jun Hatakeyama, Masayoshi Sagehashi, Takeru Watanabe
  • Patent number: 8178127
    Abstract: The subject invention provides a pharmaceutical composition comprising N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide or the salt thereof; a pharmaceutically acceptable carrier; and not more than 0.5% w/w relative to N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide of 2-Chloro-6-(1-ethyl-N-methyl-2-oxoindoline-3-carboxamido)benzoic acid, 1H,3H-spiro[5-chloro-1-methylquinoline-2,4-dione-3,3?-[1]ethylindolin-[2]-one], or 5-Chloro-N-ethyl-3-hydroxy-1-methyl-2,4-dioxo-N-phenyl-1,2,3,4-tetrahydro-quinoline-3-carboxamide.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: May 15, 2012
    Assignee: Teva Pharmaceuticals Industries, Ltd.
    Inventors: Muhammad Safadi, Daniella Licht, Ioana Lovinger, Aharon M. Eyal, Tomas Fristedt, Karl Jansson
  • Publication number: 20120115842
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein substituents A, B, X and Y are defined as in claim 1, medicaments containing said derivatives, and the use thereof in the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
    Type: Application
    Filed: December 30, 2005
    Publication date: May 10, 2012
    Inventors: Wilfried Lubisch, Thorsten Oost, Liliane Unger, Wilfried Hornberger, Herve Geneste
  • Publication number: 20120022252
    Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) methods of using such phosphacycle ligands in bond forming reactions; and (c) methods of preparing phosphacycle ligands.
    Type: Application
    Filed: July 15, 2011
    Publication date: January 26, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
  • Publication number: 20120004165
    Abstract: Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments The invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R10, X, n, B1, B2, B3 and B4 are each defined as specified, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Application
    Filed: June 7, 2011
    Publication date: January 5, 2012
    Applicant: SANOFI
    Inventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
  • Patent number: 8058269
    Abstract: There is provided compounds of the formula wherein R6, V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents.
    Type: Grant
    Filed: September 17, 2007
    Date of Patent: November 15, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Li Chen, Song Yang, Jing Zhang, Zhuming Zhang
  • Publication number: 20110275689
    Abstract: The present invention relates to novel intermediates and further to the use of said intermediates in processes for the preparation of indolinone derivatives, in particular 3-pyrrole substituted 2-indolinones having amide moieties on the pyrrole ring. Such compounds are useful in die treatment of abnormal cell growth, such as cancer, in mammals.
    Type: Application
    Filed: July 1, 2009
    Publication date: November 10, 2011
    Applicant: GENERICS [UK] LIMITED
    Inventors: Abhay Gaitonde, Bharati Choudhari, Prakash Bansode, Sunanda Phadtare
  • Publication number: 20110275832
    Abstract: Process for preparing 1,3-dihydro-2H-indol-2-ones, starting from thioalkyl-, or thiocycloalkyl-substituted indol-2-one compounds, involving a) dissolving or suspending the thioalkyl-, or thiocycloalkyl-substituted indol-2-one compounds in a polar solvent, b) adding a sulfur-containing salt to the solution or suspension, and c) heating the reaction mixture under reflux at a temperature which corresponds at most to the boiling temperature of the solvent. Use of the inventively prepared 1,3-dihydro-2H-indol-2-one as intermediates for the synthesis of fine chemicals and active ingredients from pharmacy and/or agriculture.
    Type: Application
    Filed: May 9, 2011
    Publication date: November 10, 2011
    Applicant: Bayer CropScience AG
    Inventors: Konrad Siegel, Gunter Karig
  • Publication number: 20110269812
    Abstract: The present invention relates generally to organic chemistry, biochemistry, pharmacology and medicine. More particularly, it relates to 3-benzylidene-indolin-2-one derivatives and their physiologically acceptable salts and prodrugs which modulate the activity of protein kinases (“PKs”), especially protein tyrosine kinase, and, therefore, are expected to exhibit a salutary effect against disorders related to abnormal PK activity. The present invention is further directed to methods of using of these compounds, alone or in combination with other therapeutic agents, for the alleviation, prevention and/or treatment of protein kinase-mediated diseases and disorders, such as cancer.
    Type: Application
    Filed: October 14, 2009
    Publication date: November 3, 2011
    Applicants: Agency for Science, Technology and Research, National University of Singapore
    Inventors: Mei Lin Go, Han Kiat Ho, Wei Zhang
  • Publication number: 20110263670
    Abstract: The present invention relates to novel polymorphs of sunitinib free base designated form II and form III and to processes for their preparation. The invention also relates to their use as APIs and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising said novel polymorphs and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer.
    Type: Application
    Filed: August 24, 2009
    Publication date: October 27, 2011
    Inventors: Vinayak Gore, Bharati Choudhari, Mahesh Hublikar, Prakash Bansode
  • Publication number: 20110263565
    Abstract: The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: July 28, 2009
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias Treu, Thomas Karner, Ulrich Reiser